Tolperisone hydrochloride

Biocalm®, Muscodol®, Mydeton®, Mydocalm®, Myolax®, Myoxan®, Viveo®
A Non-Selective NaV Channel Blocker
Cat #: T-115
Alternative Name Biocalm®, Muscodol®, Mydeton®, Mydocalm®, Myolax®, Myoxan®, Viveo®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 281.82
    Purity: >98%
    Effective concentration 50 µM - 2 mM.
    Chemical name 2-Methyl-1-(4-methylphenyl)-3-(1-piperidyl)propan-1-one hydrochloride.
    Molecular formula C16H23NO•HCl.
    CAS No.: 3644-61-9.
    Activity Tolperisone is a centrally acting muscle relaxant1 used for the treatment of chronic pain2. It is a Nachannel blocker with an IC50 value of 198 μM in dorsal root ganglion (DRG) cells3. It acts, at micromolar concentrations, as an acute blocker of seven different isoforms of NaV expressed in Xenopus oocytes4.
      • Bajaj, P. et al. (2003) Eur. J. Pain 7, 407.

      • Meilinger, M. et al. (2003) Annals of the Rheumatic Diseases 62, 295.

      • Kocsis, P. et al. (2005) J. Pharmacol. Exp. Ther. 315, 1237.

      • Hofer, D. et al. (2006) Eur. J. Pharmacol. 538, 5.

    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Water. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
      • Alomone Labs Tolperisone hydrochloride inhibits NaV1.2 channels expressed in Xenopus oocytes.
        A. Time course of current reversible inhibition by 0.2 mM and 1 mM Tolperisone hydrochloride (#T-115). Currents were elicited by a voltage step to 20 mV (100 ms) every 10 seconds from a holding potential of -80 mV. B. Example traces of current response to voltage step application before and during 1 mM Tolperisone hydrochloride application.
      • Amir, E. et al. (2006) J. Pain 7, S1.
      • Bajaj, P. et al. (2003) Eur. J. Pain 7, 407.
      • Meilinger, M. et al. (2003) Annals of the Rheumatic Diseases 62, 295.
      • Pratzel, H.G. et al. (1996) Pain. 67, 417.
      • Dulin, J. et al. (1998) J. Pharmacopsychiatry 31, 37.
      • Sakaue, A. et al. (2004) J. Pharmacol. Sci. 95, 181.
      • Svensson, P. et al. (2003) Eur. J. Pain 7, 449.
      • Hofer, D. et al. (2006) Eur. J. Pharmacol. 538, 5.
      • Quasthoff, S. et al. (2003) Neurosci. Lett. 352, 93.
      • Chung, J. M. et al. (2004) Novartis Found. Symp. 261, 19.
      • Kocsis, P. et al. (2005) J. Pharmacol. Exp. Ther. 315, 1237.
      • Voltage-gated Na+ channels (VGSC, NaV) are critically important for electrogenesis and nerve impulse conduction. Certain Na+ channel isoforms are predominantly expressed in peripheral sensory neurons associated with pain sensation, and the expression and functional properties of NaV in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation1.

        Tolperisone is a centrally acting muscle relaxant (muscle relaxant acting on spasticity by interaction with upper motor neurons), which is also used for the treatment of chronic pain2-3. It is mainly used for treating muscle spasticities of neurological origin and painful muscle spasms due to rheumatologic conditions. Besides being an effective antispastic agent4-5, tolperisone also has analgesic activity in rodents6 and in humans7. It possesses relatively few side effects in humans5.

        Tolperisone is an ion channel blocker that acts, at micromolar concentrations, as an acute blocker of seven different isoforms of NaV expressed in Xenopus oocytes. The drug concentrations needed to exert 50% block differ between the different isoforms are 116, 802, 96, 131, 326, 394 and 49 µM for NaV1.2, NaV1.3, NaV1.4, NaV1.5, NaV1.6, NaV1.7 and NaV1.8 channel, respectively8,9. NaV1.8, which is the most prominently affected channel, is known to be upregulated in an animal model of neuropathic pain10. The inhibitory effect is reversible and develops rapidly, with an IC50 value of 198 µM in dorsal root ganglion (DRG) cells11.

    Target NaV channels
    Last update: 11/03/2019

    Tolperisone hydrochloride (#T-115) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use